4F4P

SYK in COMPLEX WITH LIGAND LASW836

Summary for 4F4P

• Entry DOI: 10.2210/pdb4f4p/pdb
• Descriptor: Tyrosine-protein kinase SYK, N-{6-[3-(piperazin-1-yl)phenyl]pyridin-2-yl}-4-(trifluoromethyl)pyridin-2-amine, SULFATE ION, ... (4 entities in total)
• Functional Keywords: tyrosine-protein kinase, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cell membrane : P43405
• Total number of polymer chains: 1
• Total formula weight: 32088.89

Authors

Lopez, M.,Segarra, V.,Vidal, B.,Wenzkowski, C.,Jestel, A.,Krapp, S.,Blaesse, M.,Nagel, S.,Schreiner, P. (deposition date: 2012-05-11, release date: 2012-12-12, Last modification date: 2024-02-28)

Primary citation

Castillo, M.,Forns, P.,Erra, M.,Mir, M.,Lopez, M.,Maldonado, M.,Orellana, A.,Carreno, C.,Ramis, I.,Miralpeix, M.,Vidal, B.
Highly potent aminopyridines as Syk kinase inhibitors.
Bioorg.Med.Chem.Lett., 22:5419-5423, 2012

PubMed Abstract: A novel class of potent Syk inhibitors has been developed from rational design. Highly potent aminopyridine derivatives bearing a 4-trifluoromethyl-2-pyridyl motif and represented by compound 13b IC(50): 0.6 nM were identified. Substitution by a 2-pyrazinyl motif and SAR expansion in position 4 of the central core provided diverse potent non-cytotoxic Syk inhibitors showing nanomolar activity inhibiting human mast cell line LAD2 degranulation.

PubMed: 22877633
DOI: 10.1016/j.bmcl.2012.07.045

Experimental method

X-RAY DIFFRACTION (2.37 Å)